The P 2′ residue is a key determinant of mesotrypsin specificity: Engineering a high-affinity inhibitor with anticancer activity

Biochemical Journal

Volumn 440, Issue 1, 2011, Pages 95-105

  Salameh, Moh'd A ^a   Soares, Alexei S ^b   Hockla, Alexandra ^a   Radisky, Derek C ^a   Radisky, Evette S ^a  

^a MAYO CLINIC   (United States)

^b BROOKHAVEN NATIONAL LABORATORY   (United States)

Author keywords

Crystal structure; Drug discovery; Endopeptidase; Enzyme inhibition; Mesotrypsin; Protease inhibitor; Protein engineering

Indexed keywords

AMYLOID PRECURSOR PROTEIN; APROTININ; SERINE PROTEINASE INHIBITOR; ANTINEOPLASTIC AGENT; APP PROTEIN, HUMAN; PRSS3 PROTEIN, HUMAN; TRYPSIN; TRYPSIN INHIBITOR;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL; CANCER GROWTH; CANCER INVASION; CATALYSIS; CELL INVASION; CONTROLLED STUDY; CRYSTAL STRUCTURE; HUMAN; HUMAN CELL; MUTAGENESIS; PRIORITY JOURNAL; BREAST TUMOR; CHEMISTRY; DRUG DEVELOPMENT; ENZYME SPECIFICITY; FEMALE; GENETICS; METABOLISM; METHODOLOGY; PANCREAS TUMOR; PROTEIN ENGINEERING; THERMODYNAMICS; TUMOR CELL CULTURE; X RAY CRYSTALLOGRAPHY;

BOVINAE;

AMYLOID BETA-PROTEIN PRECURSOR; ANTINEOPLASTIC AGENTS; APROTININ; BREAST NEOPLASMS; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; FEMALE; HUMANS; NEOPLASM INVASIVENESS; PANCREATIC NEOPLASMS; PROTEIN ENGINEERING; SUBSTRATE SPECIFICITY; THERMODYNAMICS; TRYPSIN; TRYPSIN INHIBITORS; TUMOR CELLS, CULTURED;

EID: 80054909439     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20110788     Document Type: Article

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